Based on the well known biological versatility of the imidazoline nucleus, we prepared the novel derivatives 3a-k inspired by 2-BFI scaffold to assess imidazoline molecules as D(2)-like dopamine receptor ligands. Conservative chemical modifications of the lead structure, such as the introduction of an hydroxy group in the aromatic ring alone or associated with N-benzyl substitution, provided partial (3f) or nearly full (3e and 3h) agonists, all endowed with D(2)-like potency comparable to that of dopamine.
|Autori:||GIORGIONI G; AMBROSINI D; VESPRINI C; HUDSON A; NASUTI C; DI STEFANO A; SOZIO P; CIAMPI O; COSTA B; MARTINI C; CARRIERI A; CARBONARA G; ENZENSPERGER C; PIGINI M|
|Titolo:||Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI|
|Anno del prodotto:||2010|
|Appare nelle tipologie:||1.1 Articolo in rivista|